Chew Nora Y K, Chan Hak-Kim
Faculty of Pharmacy, University of Sydney, Sydney, Australia.
J Aerosol Med. 2002 Fall;15(3):325-30. doi: 10.1089/089426802760292672.
Pharmaceutical aerosol delivery is undergoing dramatic changes in both inhaler device and formulation aspects. There is a rapid move from the traditional propellant-driven metered dose inhalers to the high performance liquid atomizers and dry powder inhalers (DPIs). DPIs involving the dispersion of powders into aerosols by an inhaler device are particularly attractive as dry powders generally have greater chemical stability than liquids used in atomizers. Delivery of therapeutic proteins as dry powder aerosols is of high commerical interest. However, production and formulation of dry powders for inhalation can be difficult and challenging due to the potential physical instability of the powder. Dry powders consisting of micro- or nano-sized particles are inherently adhesive and cohesive, leading to highly variable dose accuracy and poor aerosol performance. Particle engineering via the use of appropriate pharmaceutical excipients and processing parameters can produce particles of optimal morphologies and surface properties which would enhance aerosol generation. Some of the key determinants for successful dispersion of pharmaceutical powders suitable for inhalation are reviewed with an emphasis on the practical significance.
药物气雾剂递送在吸入器装置和制剂方面都在经历巨大变化。从传统的推进剂驱动定量吸入器迅速转向高性能液体雾化器和干粉吸入器(DPI)。通过吸入器装置将粉末分散成气雾剂的干粉吸入器特别有吸引力,因为干粉通常比雾化器中使用的液体具有更高的化学稳定性。将治疗性蛋白质作为干粉气雾剂递送具有很高的商业价值。然而,由于粉末潜在的物理不稳定性,吸入用干粉的生产和制剂可能困难且具有挑战性。由微米或纳米级颗粒组成的干粉本质上具有粘性和内聚性,导致剂量准确性高度可变和气雾剂性能不佳。通过使用合适的药用辅料和加工参数进行颗粒工程可以产生具有最佳形态和表面性质的颗粒,这将增强气雾剂的产生。本文综述了适合吸入的药物粉末成功分散的一些关键决定因素,并强调了其实际意义。